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Anti-CD40LG (Ruplizumab)-SMCC-DM1 ADC (ADC-W-914)

This ADC product is comprised of an anti-CD40LG monoclonal antibody conjugated via a SMCC linker to DM1. The DM1 is targeted to certain cancers by immunerecognition and delivered into cancer cells via receptor mediated endocytosis. Within the cell, DM1 binds to tubulins, interrupts microtubule dynamics, and subsequently, induces cell death.

 ADC Target

  • Name
  • CD40LG
  • Alternative Names
  • CD40LG; CD40 ligand; HIGM1, IMD3, TNFSF5, tumor necrosis factor (ligand) superfamily, member 5 (hyper IgM syndrome); CD40 antigen ligand; CD40L; CD154; gp39; hCD40L; hyper IgM syndrome; T B cell activating molecule; TNF related activation protein; TRAP; tumor necrosis factor (ligand) superfamily member 5; CD40-L; T-cell antigen Gp39; T-B cell-activating molecule; TNF-related activation protein; IGM; IMD3; HIGM1; T-BAM; TNFSF5;
  • Target Entrez Gene ID
  • 959
  • Overview
  • The protein encoded by this gene is expressed on the surface of T cells. It regulates B cell function by engaging CD40 on the B cell surface. A defect in this gene results in an inability to undergo immunoglobulin class switch and is associated with hyper-IgM syndrome.

 ADC Antibody

  • Overview
  • Humanized Anti-CD40L IgG1-kappa antibody, Ruplizumab
  • Generic name
  • Ruplizumab
  • Host animal
  • Mouse
  • Species Reactivity
  • Human

 ADC Linker

  • Name
  • SMCC (N-succinimidyl 4-(Nmaleimidomethyl)cyclohexane-1-carboxylate)
  • Description
  • Disulfide Linkers, are extensively exploited as a chemically labile linkage. Since the release of disulfide-linked drugs requires a cytoplasmic thiol cofactor, such as glutathione (GSH). Disulfides maintain stable at physiological pH and only when ADCs are internalized inside cells, the cytosol provides reducing environment including intracellular enzyme protein disulfide isomerase, or similar enzymes, drugs can be released.

 ADC payload drug

  • Name
  • DM1 (N2'-Deacetyl-N2'-(3-mercapto-1-oxopropyl)maytansine)
  • Description
  • Derived from Maytansinoid,a group of cytotoxins structurally similar to rifamycin, geldanamycin, and ansatrienin. The eponymous natural cytotoxic agent maytansine is a 19-member lactam (ansa macrolide) structure originally isolated from the Ethiopian shrub Maytenus ovatus. Maytansinoids can bind to tubulin at or near the vinblastine-binding site, which interfere the formation of microtubules and depolymerize already formed microtubules, inducing mitotic arrest in the intoxicated cells.

For Research Use Only. NOT FOR CLINICAL USE.

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